Diclofenac-Grotex injection solution 75mg 3ml ampoules 3ml N5
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Active ingredients
Diclofenac
Composition
Diclofenac sodium 25 mg per 1 ml. Excipients: mannitol - 6 mg, propylene glycol - 200 mg, benzyl alcohol - 40 mg, sodium disulfite - 0.6 mg, sodium hydroxide solution 1M - to pH 7.8-8.8, water d / and - to 1 ml.
Pharmacological effect
NSAID, a derivative of phenylacetic acid. It has a pronounced anti-inflammatory, analgesic and moderate antipyretic effect. The mechanism of action is associated with inhibition of the activity of COX - the main enzyme in the metabolism of arachidonic acid, which is a precursor of prostaglandins, which play a major role in the pathogenesis of inflammation, pain and fever. The analgesic effect is due to two mechanisms: peripheral (indirectly, through suppression of prostaglandin synthesis) and central (due to inhibition of prostaglandin synthesis in the central and peripheral nervous system). Inhibits the synthesis of proteoglycan in cartilage. In rheumatic diseases it reduces joint pain at rest and during movement, as well as morning stiffness and swelling of the joints, and contributes to an increase in the range of motion. Reduces post-traumatic and postoperative pain, as well as inflammatory edema. Suppresses platelet aggregation. With prolonged use has a desensitizing effect. When applied topically in ophthalmology, it reduces swelling and pain in inflammatory processes of non-infectious etiology.
Pharmacokinetics
After ingestion is absorbed from the gastrointestinal tract. Food intake slows down the rate of absorption, the degree of absorption does not change. About 50% of the active substance is metabolized during the "first pass" through the liver. When administered rectally, absorption is slower. The time to reach Cmax in the plasma after oral administration is 2-4 hours, depending on the dosage form used, after rectal administration - 1 hour, intramuscular injection - 20 minutes. The concentration of the active substance in the plasma is linearly dependent on the magnitude of the applied dose. Does not accumulate. Plasma protein binding is 99.7% (mainly albumin). Penetrates into synovial fluid, Cmax is achieved 2-4 hours later than in plasma. It is largely metabolized to form several metabolites, among which two are pharmacologically active, but to a lesser extent than diclofenac. The systemic clearance of the active substance is approximately 263 ml / min. T1 / 2 from plasma is 1-2 hours, from synovial fluid - 3-6 hoursApproximately 60% of the dose is excreted as metabolites by the kidneys, less than 1% is excreted in the urine unchanged, the rest is excreted in the form of metabolites with bile.
Indications
Articular syndrome (rheumatoid arthritis, osteoarthritis, ankylosing spondylitis, gout), degenerative and chronic inflammatory diseases of the musculoskeletal system (osteochondrosis, osteoarthritis, periarthropathy), post-traumatic inflammation of soft tissues and musculoskeletal system (elongation). Pain in the spine, neuralgia, myalgia, arthralgia, pain and inflammation after operations and injuries, pain in gout, migraine, algomenorrhea, pain in adnexitis, proctitis, colic (biliary and renal), pain in infectious and inflammatory diseases of the ENT -organs For local use: inhibition of miosis during cataract surgery, prevention of cystoid macular edema associated with the removal and implantation of the lens, inflammatory processes of the eye of non-infectious nature, post-traumatic inflammatory process with penetrating and non-penetrating injuries of the eyeball.
Contraindications
Erosive and ulcerative lesions of the gastrointestinal tract in the acute phase, aspirin triad, impaired blood formation of unknown etiology, hypersensitivity to diclofenac and components of the dosage form used, or other NSAIDs.
Use during pregnancy and lactation
Use during pregnancy and lactation is possible in cases where the intended benefit to the mother outweighs the potential risk to the fetus or newborn.
Dosage and administration
For oral administration for adults, a single dose is 25-50 mg 2-3 times / day. The frequency of administration depends on the used dosage form, the severity of the disease and is 1-3 times / day, rectally - 1 time / day. For the treatment of acute conditions or the relief of exacerbation of a chronic process, apply IM in a dose of 75 mg. For children over 6 years old and adolescents, the daily dose is 2 mg / kg. Outwardly used in a dose of 2-4 g (depending on the area of the painful area) at the affected site 3-4 times / day. When used in ophthalmology, the frequency and duration of administration are determined individually.The maximum daily intake for adults when administered orally is 150 mg / day.
Side effects
On the part of the digestive system: nausea, vomiting, anorexia, pain and discomfort in the epigastric region, flatulence, constipation, diarrhea; in some cases - erosive and ulcerative lesions, bleeding and perforation of the gastrointestinal tract; rarely - abnormal liver function. When administered rectally in isolated cases, there was inflammation of the colon with bleeding, exacerbation of ulcerative colitis. From the side of the central nervous system and peripheral nervous system: dizziness, headache, agitation, insomnia, irritability, feeling tired; rarely - paresthesia, visual impairment (vagueness, diplopia), tinnitus, sleep disorders, convulsions, irritability, tremor, mental disorders, depression. From the side of the blood system: rarely - anemia, leukopenia, thrombocytopenia, agranulocytosis. On the part of the urinary system: rarely - impaired renal function; in predisposed patients, edema is possible. Dermatological reactions: rarely - hair loss. Allergic reactions: skin rash, itching; when applied in the form of eye drops - itching, redness, photosensitivity. Local reactions: in the place of intramuscular injection, burning is possible, in some cases - the formation of infiltration, abscess, necrosis of adipose tissue; with rectal administration, local irritation, the appearance of mucous secretions mixed with blood, painful defecation are possible; with external use in rare cases - itching, redness, rash, burning sensation; with topical application in ophthalmology, transient burning sensation and / or temporary blurred vision are possible immediately after instillation. With prolonged external use and / or application to extensive body surfaces, systemic side effects are possible due to the resorptive action of diclofenac.
Interaction with other drugs
With simultaneous use of antihypertensive drugs with diclofenac, it is possible to weaken their action. There are single reports of the occurrence of seizures in patients who took both NSAIDs and quinolone antimicrobials. With simultaneous use with GCS increases the risk of side effects from the digestive system.With the simultaneous use of diuretics may decrease diuretic effect. With simultaneous use with potassium-sparing diuretics may increase the concentration of potassium in the blood. With simultaneous use with other NSAIDs may increase the risk of side effects. There are reports of the development of hypoglycemia or hyperglycemia in patients with diabetes mellitus who used diclofenac simultaneously with hypoglycemic drugs. With simultaneous use with acetylsalicylic acid may decrease the concentration of diclofenac in the blood plasma. Although clinical studies have not established the effect of diclofenac on the effect of anticoagulants, isolated cases of bleeding with the simultaneous use of diclofenac and warfarin have been described. With simultaneous use may increase the concentration of digoxin, lithium and phenytoin in the blood plasma. The absorption of diclofenac from the gastrointestinal tract decreases with simultaneous use with Kolestiramine, to a lesser extent - with Colestipol. With simultaneous use may increase the concentration of methotrexate in the blood plasma and enhance its toxicity. With the simultaneous use of diclofenac may not affect the bioavailability of morphine, however, the concentration of the active metabolite of morphine may remain elevated in the presence of diclofenac, which increases the risk of side effects of the metabolite of morphine, including respiratory depression. With simultaneous use with pentazocine, a case of a large convulsive seizure has been described; with rifampicin - perhaps a decrease in the concentration of diclofenac in the blood plasma; with ceftriaxone - the excretion of ceftriaxone with bile increases; with cyclosporine - possible increase in cyclosporine nephrotoxicity.
special instructions
It is used with extreme caution in cases of liver, kidney, gastrointestinal tract history, dyspeptic symptoms, bronchial asthma, arterial hypertension, heart failure, immediately after serious surgical interventions, as well as in elderly patients. For indications of a history of allergic reactions to NSAIDs and diclofenac sulphites, they are used only in emergency cases. In the process of treatment requires systematic monitoring of liver and kidney function, peripheral blood pictures.Rectal administration is not recommended in patients with a history of anorectal disease or anorectal bleeding. Externally should be used only on intact skin. Diclofenac should be avoided in the eyes (with the exception of eye drops) or mucous membranes. Patients using contact lenses should use eye drops no earlier than 5 minutes after removing the lenses. Not recommended for use in children under 6 years. During treatment with dosage forms for systemic use, alcohol is not recommended. Impact on the ability to drive vehicles and control mechanisms During the period of treatment may decrease the speed of psychomotor reactions. If visual clarity deteriorates after applying eye drops, you should not drive a car or engage in other potentially dangerous activities.